Article
Pathology
Ibrahim H. Eissa, Reda G. Yousef, Muhammad Sami, Eslam B. Elkaeed, Bshra A. Alsfouk, Ibrahim M. Ibrahim, Dalal Z. Husein, Hazem Elkady, Ahmed M. Metwaly
Summary: This study developed and evaluated BHEPN as a potential inhibitor of VEGFR-2. The results showed that BHEPN inhibited VEGFR-2 and exhibited significant cytotoxic effects against cancer cell lines. Moreover, BHEPN was able to induce apoptosis and inhibit cell migration in HepG2 cells.
PATHOLOGY RESEARCH AND PRACTICE
(2023)
Article
Agronomy
Ze Zhang, Pengwei Sun, Jiahui Zhao, Hongyuan Zhang, Xinyao Wang, Linshan Li, Lixia Xiong, Na Yang, Yuxin Li, Zhiguang Yuchi, Zhengming Li
Summary: In this study, a series of novel nitrobenzene substituted anthranilic diamides were designed and synthesized. The compounds exhibited good insecticidal activity against Spodoptera frugiperda and showed better selectivity compared to chlorantraniliprole. Molecular docking analysis and in vitro studies suggested that these compounds may act through activating the RyR and targeting the dihydropyridine receptor.
PEST MANAGEMENT SCIENCE
(2022)
Article
Agronomy
Ze Zhang, Pengwei Sun, Jiahui Zhao, Hongyuan Zhang, Xinyao Wang, Linshan Li, Lixia Xiong, Na Yang, Yuxin Li, Zhiguang Yuchi, Zhengming Li
Summary: Novel nitrobenzene substituted anthranilic diamides were designed and synthesized with enhanced insecticidal activity and reduced harm to mammals. Molecular docking and in vitro studies revealed the binding modes and activation mechanisms of the new compounds.
PEST MANAGEMENT SCIENCE
(2022)
Review
Cell Biology
Hua-yang Fan, Zhuo-li Zhu, Hong-chun Xian, Hao-fan Wang, Bing-jun Chen, Ya-Jie Tang, Ya-ling Tang, Xin-hua Liang
Summary: Podophyllotoxin (PTOX) is a biologically active compound derived from the podophyllum plant, and its derivatives, such as etoposide and teniposide, show potential for cancer treatment. Studies have revealed that PTOX derivatives exert anticancer effects by inducing cell cycle arrest and DNA/RNA breaks. Despite the development of many derivatives, research on the interactions with downstream cancer-related signaling pathways is still limited.
FRONTIERS IN CELL AND DEVELOPMENTAL BIOLOGY
(2021)
Review
Oncology
Radka Michalkova, Ladislav Mirossay, Maria Gazdova, Martin Kello, Jan Mojzis
Summary: Despite significant progress in cancer treatment, mortality rates for some types of cancer have not decreased significantly, leading to a focus on finding novel anticancer drugs. Chalcones, precursors of flavonoid synthesis in plants, are natural compounds with pleiotropic biological effects, including anticancer properties.
Article
Chemistry, Multidisciplinary
Jin-yi Liu, Wei-qi Fu, Xiang-jin Zheng, Wan Li, Li-wen Ren, Jin-hua Wang, Cui Yang, Guan-hua Du
Summary: Avasimibe demonstrated potent anticancer effects on human glioblastoma cells by inhibiting proliferation, inducing apoptosis, and regulating multiple signaling pathways. The drug showed promising potential as a chemotherapy treatment for glioblastoma.
ACTA PHARMACOLOGICA SINICA
(2021)
Article
Pharmacology & Pharmacy
Rasel Ahmed Khan, Rajib Hossain, Pranta Roy, Divya Jain, Abu Saim Mohammad Saikat, Anik Prasad Roy Shuvo, Muhammad Akram, Walaa Fikry Elbossaty, Ishaq N. Khan, Sakshi Painuli, Prabhakar Semwal, Abdur Rauf, Muhammad Torequl Islam, Haroon Khan
Summary: This review gathered, analyzed, and summarized the literature on acteoside and its anticancer properties, finding that acteoside exhibits potent anticancer activity against different cancer cell lines and could be a strong candidate for further clinical studies.
EUROPEAN JOURNAL OF PHARMACOLOGY
(2022)
Review
Biochemistry & Molecular Biology
Dahye Yun, So Young Yoon, Soo Jung Park, Yoon Jung Park
Summary: Herbal plants enriched with isoquinoline alkaloids have been used in traditional folk medicine for their anti-inflammatory, antimicrobial, and analgesic effects. These alkaloids induce cell death through cell cycle arrest, apoptosis, and autophagy. The molecular mechanisms of these effects may involve binding to nucleic acids or proteins, enzyme inhibition, and epigenetic modulation.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2021)
Article
Biochemistry & Molecular Biology
Feng-Lung Tsai, Han-Li Huang, Mei-Jung Lai, Jing-Ping Liou, Shiow-Lin Pan, Chia-Ron Yang
Summary: The study found that MPT0G236, a pan-HDAC inhibitor, specifically targets malignant tumor cells and exhibits significant anticancer activity in human colorectal cancer cells, making it a potential candidate for colorectal cancer treatment.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Article
Chemistry, Medicinal
Siddavaram Nagini, Ramesh Nivetha, Manikandan Palrasu, Rajakishore Mishra
Summary: Nimbolide, a major limonoid constituent of neem, has garnered research attention for its anticancer properties. It has been shown to inhibit proliferation of cancer cells, overcome multidrug resistance, and enhance therapeutic outcomes. Nimbolide's ability to modulate signaling networks and molecular targets make it a valuable addition to the anticancer drug arsenal.
JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Article
Chemistry, Multidisciplinary
Marwa F. Ahmed, Atiah H. Almalki
Summary: New thiosemicarbazone derivatives were synthesized and evaluated for their anticancer activity, with compounds IIIa, IIIe, and IIIh showing promising results. Compound IIIa exhibited potent inhibitory activity against ribonucleotide reductase and induced apoptosis through activating the intrinsic apoptotic pathway.
ARABIAN JOURNAL OF CHEMISTRY
(2021)
Review
Medicine, Research & Experimental
Nasreddine El Omari, Saad Bakrim, Asaad Khalid, Mohammed Albratty, Ashraf N. Abdalla, Learn-Han Lee, Khang Wen Goh, Long Chiau Ming, Abdelhakim Bouyahya
Summary: Cancer progression is influenced by epigenetic events, with histone modification playing a key role in gene expression. Belinostat, a pan-HDAC inhibitor, has shown effectiveness in the treatment of T-cell lymphoma and solid malignancies. By indirectly promoting acetylated histone accumulation and restoring normal gene expressions, belinostat exhibits potential anti-cancer therapeutic effects through various pathways. Additionally, it has been found to increase p21WAF1, a cyclin-dependent kinase inhibitor involved in cell cycle arrest and apoptosis. Investigative trials have supported belinostat's potential as a valuable anti-cancer drug.
BIOMEDICINE & PHARMACOTHERAPY
(2023)
Review
Biochemistry & Molecular Biology
Sandra Lucia Teniente, Adriana Carolina Flores-Gallegos, Sandra Cecilia Esparza-Gonzalez, Lizeth Guadalupe Campos-Muzquiz, Sendar Daniel Nery-Flores, Raul Rodriguez-Herrera
Summary: Polyphenols are bioactive phytochemicals with various beneficial activities, including antioxidant, anti-inflammatory, immunomodulatory, and antiviral effects. Extracts from natural sources, such as pomegranate peel extract (PPE), containing polyphenols have shown potential in cancer prevention and treatment. The review summarizes recent scientific reports on the anticancer activity of polyphenols found in PPE, including their mechanisms of action in cervical cancer models.
Review
Pharmacology & Pharmacy
Kai Yuan, Xiao Wang, Haojie Dong, Wenjian Min, Haiping Hao, Peng Yang
Summary: CDK4/6 plays crucial roles in regulating the cell cycle and cancer cells, and selectively inhibiting CDK4/6 is an important strategy for cancer treatment. Several highly selective CDK4/6 inhibitors are currently in clinical trials, demonstrating a balance between anticancer efficacy and toxicity.
ACTA PHARMACEUTICA SINICA B
(2021)
Article
Medicine, Research & Experimental
Tahereh Tajik, Kaveh Baghaei, Vahid Erfani Moghadam, Naser Farrokhi, Seyed Alireza Salami
Summary: Plant-derived extracellular vesicles (EVs) have gained attention in recent years due to their proven therapeutic properties. In this study, EVs were isolated from two different chemotypes of cannabis and classified as high-CBD and low-CBD EVs. These EVs exhibited different cytotoxicity and anticancer effects. The findings suggest that CDEVs could be an ideal natural vehicle for delivering bioactive phytocannabinoids and a promising strategy in cancer management.
BIOMEDICINE & PHARMACOTHERAPY
(2022)
Article
Chemistry, Medicinal
Shuang Mei, Su Jiang, Yuting Wang, Han Jing, Peng Yang, Miao-Miao Niu, Jindong Li, Kai Yuan, Yan Zhang
Summary: This study identifies a dual-targeting peptide, AP-1, that effectively inhibits variants of concern (VOCs) of SARS-CoV-2 without impairing host cell viability. The findings suggest that AP-1 could be a promising broad-spectrum agent for treating emerging VOCs of SARS-CoV-2.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2024)
Article
Chemistry, Medicinal
Hyeonjun Lee, Ju Yeon Lee, Hyunsoo Jang, Hye Young Cho, Minhee Kang, Sang Hyun Bae, Suin Kim, Eunji Kim, Jaebong Jang, Jin Young Kim, Young Ho Jeon
Summary: By using liquid chromatography-tandem mass spectrometry and nuclear magnetic resonance experiments, we identified new chemical moieties that bind to the target sites of the protein of interest, allowing for reversible binding and protein degradation. This method has the potential to expand the application of PROTAC technology.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2024)
Article
Chemistry, Medicinal
Yingying Li, Xiyou Du, Xinru Kong, Yuelin Fang, Zhijing He, Dongzhu Liu, Hang Wu, Jianbo Ji, Xiaoye Yang, Lei Ye, Guangxi Zhai
Summary: This study proposes a novel nanoplatform based on the autophagy cascade to overcome the obstacles in chemo-immunotherapy. The platform combines chemotherapy and starvation therapy to initiate pro-death autophagy and enhance antigen presentation, while also remodeling the immunosuppressive tumor microenvironment. Furthermore, the study discovers a new therapeutic direction for the respiration inhibitor 3-bromopyruvic acid (3BP) in cancer treatment. Overall, this study offers an opportunity to improve antitumor efficacy and boost immune responses.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2024)
Article
Chemistry, Medicinal
Bingsi Wang, Mingxu Ma, Yusen Dai, Pengfei Yu, Liang Ye, Wenyan Wang, Chunjie Sha, Huijie Yang, Yingjie Yang, Yunjing Zhu, Lin Dong, Shujuan Wei, Linlin Wang, Jingwei Tian, Hongbo Wang
Summary: Breast cancer is a common malignant tumor in women, and drug resistance remains a clinical challenge. In this study, a novel compound, G-5b, was developed with potent antagonistic and degradation activities comparable to the current drug fulvestrant. G-5b also showed improved stability and solubility. Mechanistically, G-5b engages the proteasome pathway to degrade ER, inhibiting the ER signaling pathway and inducing apoptosis and cell cycle arrest. In animal models, G-5b exhibited superior pharmacokinetics and pharmacodynamics properties. Overall, G-5b is a promising long-acting SERD worthy of further investigation and optimization.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2024)
Article
Chemistry, Medicinal
Karoline B. Waitman, Larissa C. de Almeida, Marina C. Primi, Jorge A. E. G. Carlos, Claudia Ruiz, Thales Kronenberger, Stefan Laufer, Marcia Ines Goettert, Antti Poso, Sandra V. Vassiliades, Vinicius A. M. de Souza, Monica F. Z. J. Toledo, Neuza M. A. Hassimotto, Michael D. Cameron, Thomas D. Bannister, Leticia Costa-Lotufo, Joa o A. Machado-Neto, Mauricio T. Tavares, Roberto Parise-Filho
Summary: A series of hybrid inhibitors combining pharmacophores of known kinase inhibitors and benzohydroxamate HDAC inhibitors were synthesized and evaluated for their anticancer activity and pharmacokinetic properties. Compounds 4d-f exhibited promising cytotoxicity against hematological cells and moderate activity against solid tumor models. Compound 4d showed potent inhibition of multiple kinase targets and had stable interactions with HDAC and members of the JAK family. These compounds showed selective cytotoxicity with minimal effects on non-tumorigenic cells and favorable pharmacokinetic profiles.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2024)
Article
Chemistry, Medicinal
Michal Sulik, Diana Fontinha, Dietmar Steverding, Szymon Sobczak, Michal Antoszczak, Miguel Prudencio, Adam Huczynski
Summary: This study describes the synthesis of the first-in-class ivermectin derivatives obtained through derivatization of the C13 position, along with the unexpected rearrangement of the macrolide ring. These derivatives show potential for antiparasitic activity and are important for the development of new antiparasitic agents.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2024)
Article
Chemistry, Medicinal
Jun Liu, Qiu-Xian Chen, Wen-Fu Wu, Dong Wang, Si -Yu Zhao, Jia-Hao Li, Yi-Qun Chang, Shao-Gao Zeng, Jia-Yi Hu, Yu-Jie Li, Jia-Xin Du, Shu-Meng Jiao, Hai-Chuan Xiao, Qiang Zhang, Jun Xu, Jian-Fu Zhao, Hai -Bo Zhou, Yong-Heng Wang, Jian Zou, Ping-Hua Sun
Summary: A new anti-infective drug strategy has been discovered to attenuate virulence and modulate inflammation caused by drug-resistant Pseudomonas aeruginosa infections. Compound 5f inhibits biofilm formation, macrophage migration, and inflammatory response induced by P. aeruginosa, showing potential as a novel candidate against drug-resistant infections.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2024)
Article
Chemistry, Medicinal
Liuzeng Chen, Ke Wang, Lingyun Wang, Wei Wang, Lifan Wang, Jia Li, Xiaohan Liu, Mengya Wang, Banfeng Ruan
Summary: In this study, a series of novel anti-inflammatory compounds were designed and synthesized based on the natural product pterostilbene skeleton. Among them, compound 8 showed the highest activity and exhibited its effects through inhibition of pro-inflammatory cytokines by blocking the NF-KB/MAPK signaling pathway. Compound 8 also demonstrated a good relieving effect on acute colitis in mice and showed good safety in acute toxicity experiments.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2024)
Article
Chemistry, Medicinal
Si-Min Liang, Gui-Bin Liang, Hui-Ling Wang, Hong Jiang, Xian-Li Ma, Jian-Hua Wei, Ri-Zhen Huang, Ye Zhang
Summary: A series of novel multi-target antitumor agents were designed, synthesized, and evaluated. Some compounds exhibited significant antitumor activity and one compound showed excellent efficacy, limited toxicity, and low resistance. Further mechanism studies revealed that the compound exerted antitumor effects through multiple pathways.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2024)